Abstract
Background: It has been shown that curcumin (Cur) has anti-plasmodial activity; however, its weak bioavailability, rapid metabolism, and limited chemical stability have restricted its application in clinical usages. Nanostructured lipid carriers (NLCs) are a type of Drug-Delivery Systems (DDSs) whose core matrix is composed of both solid and liquid lipids.
Objective: The aim of the current study was to prepare and characterize curcumin-loaded nanostructured lipid carriers (Cur-NLC) for malaria treatment.
Methods: For producing NLC, coconut oil and cetyl palmitate were selected as a liquid and solid lipid, respectively. In order to prepare the Cur-NLC, the microemulsion method was applied. General toxicity assay on Artemia salina as well as hemocompatibility was investigated. Anti-plasmodial activity was studied on mice infected with Plasmodium berghei.
Results: The NLCs mean particle size and Polydispersity Index (PI) were 145 nm and 0.3, respectively. Further, the zeta potential of the Cur-NLC was −25 mV. The NLCs indicated a pseudo-spherical shape observed via transmission electron microscopy (TEM). The loading capacity and encapsulation efficacy of the obtained Cur-NLC were 3.1 ± 0.015% and 74 ± 3.32%, respectively. In vitro, Cur release profiles showed a sustained-release pattern up to 5 days in the synthesized Cur-NLC. The results of in vivo antiplasmodial activity against P. berghei revealed that antimalarial activity of Cur-NLC was significantly higher compared with that of free Cur at the dose of 40 mg/kg/day.
Conclusion: The results of this study suggested that NLC would be used as a potential nanocarrier for the treatment of malaria.
Keywords: Nanostructured lipid carriers (NLCs), Curcumin, Malaria, Plasmodium berghei, Drug-Delivery Systems (DDSs), Polydispersity Index (PI).
Graphical Abstract
[http://dx.doi.org/10.3390/tropicalmed4020089] [PMID: 31167396]
[http://dx.doi.org/10.1016/j.bbrc.2004.11.051] [PMID: 15582601]
[http://dx.doi.org/10.1021/nn405077y] [PMID: 24467380]
[http://dx.doi.org/10.1016/j.matchemphys.2018.12.089]
[http://dx.doi.org/10.1016/j.phrs.2019.01.020] [PMID: 30641277]
[http://dx.doi.org/10.1002/ptr.5984] [PMID: 29168312]
[http://dx.doi.org/10.1007/s00280-013-2151-8] [PMID: 23543271]
[http://dx.doi.org/10.1016/j.ijpharm.2015.06.022] [PMID: 26189427]
[http://dx.doi.org/10.1007/s11164-018-3593-8]
[http://dx.doi.org/10.1016/j.msec.2015.12.067] [PMID: 26838895]
[http://dx.doi.org/10.1016/j.msec.2019.03.004] [PMID: 30948114]
[PMID: 26957282]
[http://dx.doi.org/10.2174/157016311796799062] [PMID: 21291409]
[http://dx.doi.org/10.1016/j.foodres.2011.09.025]
[http://dx.doi.org/10.1186/1476-511X-11-159] [PMID: 23167765]
[PMID: 25367836]
[http://dx.doi.org/10.1515/acph-2017-0021] [PMID: 28858837]
[http://dx.doi.org/10.1016/j.tips.2015.09.007] [PMID: 26521094]
[http://dx.doi.org/10.1021/mp700113r] [PMID: 17999464]
[http://dx.doi.org/10.1039/C5RA19793G]
[http://dx.doi.org/10.1080/10717540601036880] [PMID: 17497352]
[http://dx.doi.org/10.1021/jf305143k] [PMID: 23362941]
[http://dx.doi.org/10.1186/s40199-015-0105-x] [PMID: 25888940]
[http://dx.doi.org/10.1111/j.1744-7348.1949.tb06408.x] [PMID: 18151945]
[http://dx.doi.org/10.1016/j.ijpddr.2015.03.002] [PMID: 25949928]
[http://dx.doi.org/10.18502/jad.v12i2.39] [PMID: 30123807]
[http://dx.doi.org/10.1080/10837450.2017.1372781] [PMID: 28851256]
[http://dx.doi.org/10.1016/j.exppara.2010.01.005] [PMID: 20093114]
[http://dx.doi.org/10.1016/S0378-5173(02)00269-7] [PMID: 12176302]
[http://dx.doi.org/10.1021/ja107583h] [PMID: 21288025]
[PMID: 21699068]
[http://dx.doi.org/10.18388/abp.2012_2139] [PMID: 22590694]
[http://dx.doi.org/10.14227/DT170310P24]
[http://dx.doi.org/10.1016/j.colsurfb.2005.08.005] [PMID: 16198092]
[http://dx.doi.org/10.1016/j.ejpb.2007.01.015] [PMID: 17346953]
[http://dx.doi.org/10.1023/A:1016042504830] [PMID: 8893284]
[http://dx.doi.org/10.1055/s-2007-971236] [PMID: 17396775]